YM 298198 hydrochloride

Discontinued Product

YM 298198 hydrochloride (Cat. No. 2448) has been withdrawn from sale for commercial reasons.
Description: Highly potent, selective non-competitive mGlu1 antagonist
Chemical Name: 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (5)

Biological Activity for YM 298198 hydrochloride

YM 298198 hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM); inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). Inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively), and is orally active in vivo, demonstrating an antinociceptive effect in hyperalgesic mice.

Desmethyl Derivative also available.

Licensing Information

Sold with the permission of Astellas Pharma Inc.

Technical Data for YM 298198 hydrochloride

M. Wt 378.92
Formula C18H22N4OS.HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 1216398-09-2
PubChem ID 45073464
InChI Key WYTJVUVCSUWZTH-UHFFFAOYSA-N
Smiles Cl.CN(C1CCCCC1)C(=O)C1=C(C)N2C(S1)=NC1=CC=C(N)C=C21

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for YM 298198 hydrochloride

References for YM 298198 hydrochloride

References are publications that support the biological activity of the product.

Kohara et al (2005) Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective and noncompetitive antagonist of metabo J.Pharmacol.Exp.Ther. 315 163 PMID: 15976016

Emery et al (2010) The protective signaling of metabotropic glutamate receptor 1 is mediated by sustained, β-arrestin-1-dependent ERK phosphorylation. J.Biol.Chem. 285 26041 PMID: 20566651

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1 Citation for YM 298198 hydrochloride

Citations are publications that use Tocris products. Selected citations for YM 298198 hydrochloride include:

Yasuda et al (2018) Drebrin Isoforms Critically Regulate NMDAR- and mGluR-Dependent LTD Induction. Front Cell Neurosci 12 330 PMID: 30349460


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Metabotropic Glutamate Receptors Scientific Review

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.

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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

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Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.

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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.